Effect of GnRH Active Immunisation on Reproductive Performance of Male Sprague Dawley Rats.

To investigate the effect of active immunisation with gonadotropin-releasing hormone (GnRH) on the reproductive function in male Sprague Dawley (SD) rats, 24 42-day-old rats were randomly assigned to treatment with GnRH6-MAP, GnRH-OVA, a surgical castration group, and a blank control group. Each rat in the treatment groups was intramuscularly injected at 6, 8, and 10 weeks of age. The serum concentrations of testosterone (T), follicle-stimulating hormone (FSH), luteinising hormone (LH), and anti-GnRH antibodies were determined using enzyme-linked immunosorbent assays. The results showed that active immunisation with recombinant GnRH6-MBP and GnRH-OVA significantly increased the serum levels of anti-GnRH antibodies and reduced the serum concentrations of testosterone compared to the black control. Eight weeks after immunisation, the rats' testes were surgically removed for morphological evaluation, showing atrophy of the convoluted vasculature, relative emptying of the lumen, and insignificant differentiation of spermatogonial cells, which were increased in weight and volume compared with the blank control group. These findings indicated that active immunisation with GnRH can lead to testicular atrophy and reduce gonadal hormone concentrations, suggesting that GnRH is a highly effective immunogen.

Palladium- and nickel-catalyzed cascade enantioselective ring-opening/coupling reactions of cyclobutanones.

The chemistry of small ring compounds is an intriguing subject in organic chemistry. As the smallest stable cyclic aliphatic ketones, cyclobutanones have garnered tremendous attention owing to their intrinsic high reactivity such as transition-metal catalyzed C-C bond cleavage. In this context, transition-metal catalyzed formal cycloaddition of cyclobutanones via a "cut and sew" strategy has gained marvelous advances. In contrast, an alternative reaction paradigm, i.e., transition-metal catalyzed ring-opening reactions of cyclobutanones, is still underdeveloped. This feature article aims to summarize our efforts in developing enantioselective palladium-catalyzed ring-opening/coupling reactions and recently emerging nickel-catalyzed ring-opening/reductive coupling reactions of cyclobutanones with a tethered aryl halide. The possible mechanisms are briefly showcased and the advantages and limitations of each strategy as well as their synthetic applications in the synthesis of natural products or bioactive compounds are presented.

Administration of USP7 inhibitor P22077 inhibited cardiac hypertrophy and remodeling in Ang II-induced hypertensive mice.

Hypertension is one of the common causes of pathological cardiac hypertrophy and a major risk for morbidity and mortality of cardiovascular diseases worldwide. Ubiquitin-Specific Protease 7 (USP7), the first identified deubiquitinating enzymes, participated in a variety of biological processes, such as cell proliferation, DNA damage response, tumourigenesis, and apoptosis. However, its role and mechanism in cardiac remodeling remain unclear. Here, our data indicated that USP7 expression was increased during Ang II-induced cardiac hypertrophy and remodeling in mice and humans with heart failure, while the administration of its inhibitor p22077 attenuated cardiac hypertrophy, cardiac fibrosis, inflammation, and oxidase stress. Mechanistically, the administration of p22077 inhibited the multiple signaling pathways, including AKT/ERK, TGF-ß/SMAD2/Collagen I/Collagen III, NF-κB/NLRP3, and NAPDH oxidases (NOX2 and NOX4). Taken together, these findings demonstrate that USP7 may be a new therapeutic target for hypertrophic remodeling and HF.

Application of aromatic amide-derived atropisomers as chiral solvating agents for discrimination of optically active mandelic acid derivatives in 1 H nuclear magnetic resonance spectroscopy.

Non-biaryl atropisomers and their stereochemistry have attracted much attentions in the past years. However, application of the non-biaryl atropisomers as chiral solvating agents is yet to be explored. In this work, four aromatic amide-derived atropisomeric phosphine ligands (hosts) were used as chiral solvating agents to recognize various mandelic acid derivatives (guests) in 1 H nuclear magnetic resonance (NMR) spectroscopy. It is found that chiral center configurations of the four hosts have different effects on the enantiorecognition to the used guests. In addition, the host and guest interaction was further investigated by determination of the host-guest complex stoichiometry using the Job's method and density functional theory calculation, respectively. Moreover, chiral analysis accuracy of these hosts was evaluated through relationship between enantiomeric excess values of 4-chloromandelic acid provided by NMR and gravimetry, respectively.

[Effects of abrupt salinity stress on osmoregulation of juvenile Rachycentron canadum].

Rachycentron canadum is a thriving mariculture species for offshore cage in southern Mainland and Taiwan of China, due to its rapid growth rate and high quality flesh. In this paper, the gill Na(+)-K+ ATPase (NKA) activity and iono- and osmoregulation of juvenile R. canadum were investigated in a 12 h stress of ambient salinities (0-45), and the results showed that after an abrupt transfer to the salinities of 0, 5, 15, 25, 37 (control) and 45, the death of juvenile R. canadum only occurred in salinity 0, with a mortality of 100% by the end of the experiment. In all treatments, the gill NKA activity and serum osmolality fluctuated in first 3 h, and then changed smoothly. The NKA activity varied with salinity grade in U shape, being significantly (P < 0.05) higher in salinity 5 and the lowest in salinity 15 in 12 h, while the serum osmolality (ranged 293-399 mOsmol x kg(-1)) presented a positive correlation with salinity. Serum [Na+] and [Cl-] concentration slightly increased with salinity within the period of 3-12 h, while serum [K+] displayed a reverse pattern. The isosmotic point was estimated as 328.2 mOsm x kg(-1) and corresponded to salinity 11.48. The isoionic points for serum [Na+], [K+] and [Cl-] were estimated as 155.2, 6.16, and 137.1 mmol x L(-1), which corresponded to the salinities of 10.68, 20.44 and 8.41, respectively. It was concluded that R. canadum could be characterized physiologically as a "higher-NKA-in-hyposmotic media" marine euryhaline teleost with the capability of rapid and effective hyper/hypo iono- and osmoregulation.